cxcr4-in-1

CXCR4-IN-1 (Example C5) 为CXCR4抑制剂，IC50值为20 nM。该化合物主要适用于癌症、HIV、糖尿病视网膜病变、炎症等领域的研究。

Oroxylin A (Baicalein 6-methyl ether) 是一种有活性的黄酮，具有较强的抗癌作用。

IT1t dihydrochloride 抑制 CXCL12 CXCR4 相互作用，IC50 为 2.1 nM。 IT1t dihydrochloride 是 CXCR4 的拮抗剂。

Arylsulfonamide 64B (HIF inhibitor 64B) 作为一种有效的缺氧诱导因子 (hypoxia induced factor, HIF) 抑制剂，通过抑制缺氧 HIF 诱导的 c-Met 和 CXCR4 的表达，能显著降低葡萄膜黑色素瘤小鼠模型中原发肿瘤的生长与转移。

ATI-2341 is an effective functionally selective allosteric agonist for the c-x-c chemokine receptor type 4 (CXCR4), which ACTS as a biased ligand in favor of G G G G G 1 activation instead of G G G G G 13.ATI-2341 activates the inhibitory heterotrimer G p

AMD-3329 hydrobromide is a biochemical in the class of potent and selective anti-HIV-1 and HIV-2 agents that inhibit virus replication by binding to the chemokine receptor CXCR4, the co-receptor for entry of X4 viruses.

Peptide R 是一种环状肽，是一种特异性 CXCR4拮抗剂。Peptide R 显示出有效的重塑肿瘤间质的出色能力。Peptide R 具有用于肿瘤研究的潜力。

CXCR4 antagonist 7 (Compound PARA-B) 是可用于研究HIV 感染、炎症性疾病、癌症和 WHIM 综合症的CXCR4拮抗剂 (IC50 = 9.3 nM)。

AMD-070 hydrochloride 是一种 CXCR4 拮抗剂，可用于抗 HIV。

Mavorixafor (AMD-070) 是一种有效的特异性 CXCR4 拮抗剂，对 CXCR4 125I-SDF 结合的 IC50 值为 13 nM。 Mavorixafor 在 MT-4 细胞 (IC50 = 1 nM) 和 PBMC (IC50 = 9 nM) 中抑制 T-tropic HIV-1 (NL4.3 株) 的复制。

AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM). However, it has no effect on CCR5-using (R5) viruses. AMD 3465 (GENZ-644494) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC

Interleukin-2-inducible T cell kinase (ITK) is a non-receptor tyrosine kinase expressed in T cells, NKT cells and mast cells which plays a crucial role in regulating the T cell receptor (TCR), CD28, CD2, chemokine receptor CXCR4, and FcepsilonR-mediated signaling pathways. ITK inhibitors can be used for the treatment of inflammation and immune-mediated disorders. ITK inhibitor (N-[5-[[3-[(4-Acetylpiperazin-1-yl)carbonyl]-4-methyl-6-methoxy-phenyl]thio]thiazol-2-yl]-4-(N-1,2-dimethylpropylaminomethyl)benzamide) is the analogue of BMS-509744, which can potently and selectively inhibit Itk kinase activity. In vitro: BMS-509744 could reduce TCR-induced functions including PLCγ1 tyrosine phosphorylation, calcium mobilization, IL-2 secretion, and T-cell proliferation in vitro in both human and mouse cells [1]. In vivo: BMS-509744 suppressed the production of IL-2 induced by anti-TCR antibody administered to mice. BMS-509744 also significantly diminishes lung inflammation in a mouse model of ovalbumin-induced allergy/asthma [1]. Clinical trial: Up to now, both BMS-509744 and ITK inhibitor is still in the preclinical development stage.

IT1t inhibits CXCL12 CXCR4 interaction with an IC50 of 2.1 nM. is a potent CXCR4 antagonist.

NoxaBH3，一种基于半胱氨酸的交联肽，具备提高的细胞渗透性及较高对Mcl-1的抑制效能。该化合物通过与CXCR4的内源性配体结合，形成泛素-NoxaBH3偶联物，进而被导向癌细胞。

CTCE-0214 是一种 CXCR4(chemokine CXC receptor 4) 激动剂，是 SDF-1α 肽类似物。CTCE-0214 具有抗炎活性，可用于炎症败血症和系统性炎症综合征的研究。

AMD-3451 free base is a dual CCR5 CXCR4 antagonist which may be useful in the treatment of a wide variety of R5, R5 X4, and X4 strains of human immunodeficiency virus type 1 (HIV-1) and HIV-2. AMD3451 is the first low-molecular-weight anti-HIV agent with selective HIV coreceptor, CCR5 and CXCR4, interaction.

CXCR4 antagonist 8 (Compound 3) is a potent inhibitor of CXCR4. It demonstrates an IC50 value of 57 nM in CXCR4 antagonism. In addition, it effectively inhibits the increase in cytosolic calcium induced by CXCL12 with an IC50 value of 0.24 nM. Furthermore, Compound 3 shows efficacy in the inhibition of CXCL12 CXCR4-mediated cell migration [1].

AMD 3465 hexahydrobromide (GENZ-644494 (hexahydrobromide)) 是一种 CXCR4受体拮抗剂，具有潜在的抗癌和抗 HIV 活性。

CXCR4-IN-2（compound A1）是一款具有抗癌活性的双功能氟化小分子，是CXCR4的强效抑制剂。它对小鼠结直肠癌(CRC)细胞展现出显著的细胞毒性（IC50：60 μg mL；72小时）和抗增殖能力，能够引导细胞在G2 M期发生阻滞并诱导细胞凋亡(apoptosis)。

NUCC-390 dihydrochloride 是新型的选择性小分子CXCR4receptor 受体激动剂。NUCC-390 dihydrochloride 可以诱导CXCR4受体的内化，作用方式与 AMD3100 相反。NUCC-390 dihydrochloride 在动物模型中，有助于神经退行性变后神经功能恢复。

KRH-1636 is an orally active, selective and extremely potent CXC chemokine receptor 4 antagonist. KRH-1636 exhibits a potent and selective anti-HIV-1 activity. KRH-1636 efficiently blocked replication of various T cell line-tropic (X4) HIV type 1 (HIV-1) in MT-4 cells and peripheral blood mononuclear cells through the inhibition of viral entry and membrane fusion via the CXC chemokine receptor (CXCR)4 coreceptor but not via CC chemokine receptor 5. KRH-1636 also inhibits binding of the CXC chemokine, stromal cell-derived factor 1alpha, to CXCR4 specifically and subsequent signal transduction. KRH-1636 prevented monoclonal antibodies from binding to CXCR4 without down-modulation of the coreceptor. KRH-1636 seems to be a promising agent for the treatment of HIV-1 infection.

SDF-1α (human) 是一种能够与CXCR4受体相结合的单核细胞趋化剂，它在心肌梗死模型中的干细胞归巢、维持、生存、增殖、心肌细胞修复、血管形成以及心室重构过程扮演关键角色。SDF-1α (human) 常用于心血管病研究。

Mavorixafor trihydrochloride is a selective and orally available CXCR4 antagonist (IC50: 13 nM against CXCR4 125I-SDF binding) and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs (IC50s: 1 and 9 nM).

CTCE-9908 TFA 是一种有效的，选择性的 CXCR4抑制剂。CTCE-9908 TFA 在表达 CXCR4的卵巢癌细胞中诱导有丝分裂突变，诱导细胞毒性，抑制迁移。